2. Cell Cycle/DNA Damage Epigenetics Anti-infection
  3. HDAC HIV
  4. BRD-6929

BRD-6929 是 I 类组蛋白去乙酰化酶 HDAC1 和 HDAC2 的脑渗透性选择性抑制剂 (IC50= 1 和 8 nM)。BRD-6929 对 HDAC1 和 HDAC2 有高亲和力 (Ki = 0.2 和 1.5 nM)。BRD-6929 可用于情绪相关行为的研究。

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BRD-6929

BRD-6929 Chemical Structure

CAS No. : 849234-64-6

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规格 价格 是否有货 数量
1 mg ￥198
In-stock
5 mg ￥590
In-stock
10 mg ￥945
In-stock
25 mg ￥1980
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50 mg ￥3180
In-stock
100 mg ￥4850
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500 mg   询价  

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BRD-6929 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 HIV 亚型特异性产品:

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HIV HIV-1 HIV-2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 and HDAC2 inhibitor with IC50 of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research[3].

IC50 & Target[1][3]

HDAC1

1 nM (IC50)

HDAC2

8 nM (IC50)

HDAC3

458 nM (IC50)

HIV-1

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Epithelial cell IC50
> 50 μM
Compound: 19
Cytotoxicity against human mammary epithelial cells by MTT assay
Cytotoxicity against human mammary epithelial cells by MTT assay
[PMID: 17941625]
HCT-116 IC50
0.5 μM
Compound: 19
Cytotoxicity against human HCT116 cells by MTT assay
Cytotoxicity against human HCT116 cells by MTT assay
[PMID: 17941625]
Jurkat CC50
12.6 μM
Compound: 1; TPB
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 29541372]
Jurkat IC50
204 nM
Compound: 1
Inhibition of FLAG-tagged HDAC1 S113A mutant (unknown origin) expressed in Jurkat cells after 2 hrs by Fluor de lys staining-based fluorimetric analysis
Inhibition of FLAG-tagged HDAC1 S113A mutant (unknown origin) expressed in Jurkat cells after 2 hrs by Fluor de lys staining-based fluorimetric analysis
[PMID: 24405391]
Jurkat IC50
40 nM
Compound: 1
Inhibition of wild-type FLAG-tagged HDAC1 (unknown origin) expressed in Jurkat cells after 2 hrs by Fluor de lys staining-based fluorimetric analysis
Inhibition of wild-type FLAG-tagged HDAC1 (unknown origin) expressed in Jurkat cells after 2 hrs by Fluor de lys staining-based fluorimetric analysis
[PMID: 24405391]
KB IC50
5.27 μM
Compound: SHI1:2
Cytotoxicity against human KB cells after 72 hrs by MTS assay
Cytotoxicity against human KB cells after 72 hrs by MTS assay
[PMID: 25899338]
Sf9 IC50
0.001 μM
Compound: 60
Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate
Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate
[PMID: 27377864]
Sf9 IC50
0.013 μM
Compound: 60
Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate preincubated for 3 hrs measured after 60 mins by flu
Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate preincubated for 3 hrs measured after 60 mins by flu
[PMID: 27377864]
U-937 CC50
14 μM
Compound: 1; TPB
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 29541372]
体外研究
(In Vitro)

使用重组人 HDAC 酶和 HDAC 类别特异性底物，BRD-6929 对 HDAC1-9 的体外 IC50。 BRD-6929 和底物孵育 180 分钟 (HDAC1-3)，BRD-6929 针对 HDAC1、HDAC2、HDAC3 和 HDAC4-9 的 IC50 分别为 0.001 μM、0.008 μM、0.458 μM 和 >30 μM[1]。
体外结合亲和力 (Ki) 和动力学 (半衰期“T1/2′ 以分钟为单位) 对于与 BRD-6929 (10 μM) 孵育的 HDAC 1、2 和 3，Ki 值分别为 <0.2 nM、1.5 nM 和 270 nM。HDAC 1、2 和 3 的 T1/2 值分别为 >2400 分钟、>4800 分钟和 1200 分钟[1]。
BRD-6929 (1 和 10 μM) 不会导致脑区特异性原代培养物中细胞总数的增加或减少。此外，BRD-6929 (10 μM) 会导致脑区特异性原代培养物(纹状体)中 H4K12 乙酰化增加[1]。
BRD-6929 (1-10 μM；6 小时) 会导致原代神经元细胞培养物中 H2B 乙酰化显著增加。BRD-6929 (1-20 μM；24 小时)诱导 H4K12ac 的剂量依赖性乙酰化，在培养的神经元中 EC50 为 7.2 μM[1]。
BRD-6929 增强了 Gnidimacrin (一种 PKC 激动剂) 对抗潜伏 HIV-1 的功效[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BRD-6929 相关抗体:
体内研究
(In Vivo)

BRD-6929 (腹膜内注射；45 mg/kg；单剂量) 在血浆中的 Cmax、T1/2 和 AUC 值分别为 17.7 μM、7.2 小时和 25.6 μM/L*hr。其在脑组织中的 Cmax、T1/2 和 AUC 值分别为 0.83 μM、6.4 小时和 3.9 μM/L*hr[1]。
BRD-6929 (腹膜内注射；45 mg/kg；10 天) 在小鼠脑组织中作为脱乙酰基酶抑制剂发挥作用。与赋形剂相比，它显著提高了各脑区乙酰化水平，达 1.5 至 2.0 倍。蛋白质印迹法检测显示，BRD-6929 在成年雄性 C57BL/6J 小鼠中连续 10 次每日治疗后，显著增加皮质、腹侧纹状体和海马中组蛋白 H2B (四乙酰化)、H3K9 和 H4K12 的乙酰化程度[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

351.42

Formula

C19H17N3O2S
CAS 号
性状

固体

颜色

Off-white to gray

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: ≥99.0%

COA (283 KB)

产品使用指南 (1538 KB)
参考文献

BRD-6929 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BRD-6929849234-64-6BRD6929BRD 6929HDACHIVHistone deacetylasesHuman immunodeficiency virusmood-relatedbehavioralHDACiInhibitorinhibitorinhibit

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